Nimodipine CAS No. 66085-59-4

Product Description

Nimodipine is a dihydropyridine calcium channel blocker specifically designed to target L-type calcium channels in the brain, primarily used to prevent and treat neurological deficits resulting from cerebral vasospasm following subarachnoid hemorrhage (SAH). It works by blocking calcium influx into vascular smooth muscle cells, leading to vasodilation of cerebral arteries and improved blood flow in ischemic brain regions. Nimodipine is most effective when administered within 96 hours of SAH onset and is typically given orally at 60 mg every 4 hours for 21 days. While it is primarily used for SAH, it has also been explored for off-label uses such as migraine prevention and vascular dementia, though evidence for these applications is limited. Common side effects include hypotension, headache, dizziness, and gastrointestinal disturbances. Nimodipine should be used with caution in patients with severe liver impairment and should not be taken with strong CYP3A4 inhibitors or grapefruit juice, which can increase drug levels.

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Product Use & Characteristics

Chemical Properties

• Molecular Formula: C₂₁H₂₆N₂O₇

• Molecular Weight: 418.4 g/mol

• IUPAC Name: 3-O-(2-methoxyethyl) 5-O-propan-2-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

• Solubility: Soluble in organic solvents; available in oral and intravenous formulations.

• Lipophilicity: High, allowing it to cross the blood-brain barrier effectively.

Mechanism of Action

• Calcium Channel Blockade: Nimodipine selectively blocks L-type calcium channels in vascular smooth muscle cells, particularly in the brain.

• Vasodilation: By inhibiting calcium influx, it causes relaxation and dilation of cerebral arteries, improving blood flow to ischemic brain regions.

• Neuroprotection: Reduces calcium-mediated neuronal damage, providing additional neuroprotective effects.

Clinical Uses

• Primary Use: Prevention and treatment of cerebral vasospasm following subarachnoid hemorrhage (SAH).

  • Efficacy: Most effective when administered within 96 hours of SAH onset.

• Off-label Uses: Investigated for migraine prevention, vascular dementia, and acute ischemic stroke, though evidence is limited.

Administration

• Oral: Preferred route; 60 mg every 4 hours for 21 days.

• Intravenous (IV): Used in patients unable to take oral medication; less common due to hypotension risk.

Side Effects

• Common:

  • Hypotension (most common)

  • Headache

  • Dizziness

  • Flushing

  • Gastrointestinal disturbances (nausea, diarrhea)

• Serious:

  • Severe allergic reactions

  • Heart rhythm problems

  • Liver dysfunction (rare)

Contraindications and Precautions

• Hypersensitivity: Known allergy to nimodipine or other dihydropyridines (e.g., nifedipine, amlodipine).

• Severe Liver Impairment: Dose adjustment may be needed.

• Intravenous Administration: Oral formulation should not be administered intravenously due to severe adverse effects (e.g., hypotension, cardiovascular collapse).

• Drug Interactions:

  • CYP3A4 Inhibitors: Avoid strong inhibitors (e.g., ketoconazole, clarithromycin) due to increased drug levels.

  • CYP3A4 Inducers: Avoid strong inducers (e.g., rifampin, carbamazepine) due to decreased drug levels.

  • Grapefruit Juice: Avoid due to increased drug levels.

• Pregnancy and Breastfeeding: Safety during pregnancy is not established; breastfeeding is generally advised against during therapy.

Monitoring and Considerations

• Blood Pressure and Heart Rate: Should be carefully monitored during treatment.

• Liver Function: Monitor in patients with liver impairment.

• Treatment Duration: Typically 21 days for SAH, starting as soon as possible after hemorrhage onset.

Brand Name

• Nimotop: Most common brand name.

Important Considerations

• Timing: Treatment should begin within 96 hours of SAH onset for optimal efficacy.

• Not Effective for Other Strokes: Not indicated for other types of strokes or general hypertension.

• Adherence: Patients should take nimodipine exactly as prescribed and inform their healthcare provider about all other medications, supplements, and pre-existing conditions.

Why us!

Qingdao Sigma Chemical Co., Ltd., established in January 2017 and headquartered in Qingdao, China, is a reliable chemical supplier. Specializing in pharmaceuticals, biochemical intermediates, and research chemicals, the company offers a diverse product portfolio, including peptides (e.g., Tirzepatide, Semaglutide), nootropics, veterinary products, and APIs, often marketed with ≥99% purity and COA certification. We provides R&D, custom synthesis, and contract manufacturing services at various scales, while claiming a global export presence across 100+ countries. With international warehouses in the USA, Europe, Australia, and Canada, Qingdao Sigma Chemical also facilitates drop-shipping and reshipments, positioning itself as a key supplier for laboratory and research applications.